کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10587791 | 981436 | 2013 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of arylglycine-based analogs was synthesized and tested for TRPM8 antagonism in a cell-based functional assay. Following structure-activity relationship studies in vitro, a number of compounds were identified as potent TRPM8 antagonists and were subsequently evaluated in an in vivo pharmacodynamic assay of icilin-induced 'wet-dog' shaking in which compound 12 was fully effective. TRPM8 antagonists of the type described here may be useful in treating pain conditions wherein cold hypersensitivity is a dominant feature.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 7, 1 April 2013, Pages 2234-2237
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 7, 1 April 2013, Pages 2234-2237
نویسندگان
Bin Zhu, Mingde Xia, Xiaoqing Xu, Donald W. Ludovici, Manomi Tennakoon, Mark A. Youngman, Jay M. Matthews, Scott L. Dax, Raymond W. Colburn, Ning Qin, Tasha L. Hutchinson, Mary Lou Lubin, Michael R. Brandt, Dennis J. Stone, Christopher M. Flores,